Log in to search using one of your social media accounts:

 

Development of hydroxyapatite nanoparticles loaded with folic acid to induce osteoblastic differentiation
Publication date: 10 January 2017 Source:International Journal of Pharmaceutics, Volume 516, Issues 1–2 Author(s): Catarina Santos, Pedro Gomes, José A. Duarte, Margarida M. Almeida, Maria E.V. Costa, Maria H. Fernandes Recently it has been shown that folic acid can have an important role in bone regeneration. For this reason, combining a classic bone regeneration system as, hydroxyapatite, loaded with folic acid, may be an important issue to be developed. To address this issue, hydroxyapatite nanoparticles loaded with folic acid were designed as an effective bone regenerative system, to induce osteoblast dif...
Source: International Journal of Pharmaceutics - November 18, 2016 Category: Drugs & Pharmacology Source Type: research

Microbial biosensors to monitor the encapsulation effectiveness of Doxorubicin in chimeric advanced Drug Delivery Nano Systems: A calorimetric approach
Publication date: 10 January 2017 Source:International Journal of Pharmaceutics, Volume 516, Issues 1–2 Author(s): Konstantinos Gardikis, Marco Signorelli, Chiara Ferrario, Alberto Schiraldi, Maria Grazia Fortina, Sophia Hatziantoniou, Costas Demetzos, Dimitrios Fessas The release of the anticancer drug doxorubicin (DOX) incorporated in a new drug carrier, namely a chimeric nanosystem formed by liposomes and dendrimers, was studied following the influence of the drug on the growth kinetics of the Lactobacillus helveticus bacterium, that would mimic the intestinal microflora. The bacterial growth was followed at 37&d...
Source: International Journal of Pharmaceutics - November 18, 2016 Category: Drugs & Pharmacology Source Type: research

Spray freeze drying as an alternative technique for lyophilization of polymeric and lipid-based nanoparticles
Publication date: 10 January 2017 Source:International Journal of Pharmaceutics, Volume 516, Issues 1–2 Author(s): Mohamed Ehab Ali, Alf Lamprecht The use of nanoparticles for drug delivery is still restricted by their limited stability when stored in an aqueous medium. Freeze drying is the standard method for long-term storage of colloidal nanoparticles; however the method needs to be elaborated for each formulation. Spray freeze drying (SFD) is proposed here as a promising alternative for lyophilizing colloidal nanoparticles. Different types of polymeric and lipid nanoparticles were prepared and characterized. Aft...
Source: International Journal of Pharmaceutics - November 18, 2016 Category: Drugs & Pharmacology Source Type: research

Biocompatibility and drug release behavior of curcumin conjugated gold nanoparticles from aminosilane-functionalized electrospun poly(N-vinyl-2-pyrrolidone) fibers
In this study, the 3-aminopropyltriethoxysilane (APTES)-functionalized electrospun poly(N-vinyl-2-pyrrolidone) fibers (NH2-PVP) were utilized as a free-standing substrate for the immobilization of CUR-PVP capped gold nanoparticles (CUR-PGNPs) conjugates. The conjugate was synthesized by sonication and the drug entrapment percentage was determined to be 54.2 ±1.8. CUR-PGNPs immobilized on NH2-PVP fibers showed a moderate burst release during the first few hours, followed by a sustained release lasting for 2days. The drug release was found pH-dependent (pH 5.0>6.0>7.4). The two-stage release profi...
Source: International Journal of Pharmaceutics - November 17, 2016 Category: Drugs & Pharmacology Source Type: research

Thermodynamics of aggregate formation between a non-ionic polymer and ionic surfactants: An isothermal titration calorimetric study
This report examines the energetics of aggregate formation between hydroxypropyl methylcellulose (HPMC) and model ionic surfactants including sodium dodecyl sulfate (SDS) at pharmaceutically relevant concentrations using the isothermal titration calorimetry (ITC) technique and a novel treatment of calorimetric data that accounts for the various species formed. The influence of molecular weight of HPMC, temperature and ionic strength of solution on the aggregate formation process was explored. The interaction between SDS and HPMC was determined to be an endothermic process and initiated at a critical aggregation concentrati...
Source: International Journal of Pharmaceutics - November 17, 2016 Category: Drugs & Pharmacology Source Type: research

The strategic relevance of manufacturing technology: An overall quality concept to promote innovation preventing drug shortage
Publication date: 10 January 2017 Source:International Journal of Pharmaceutics, Volume 516, Issues 1–2 Author(s): Michele Panzitta, Mauro Ponti, Giorgio Bruno, Giancarlo Cois, Alessandro D’Arpino, Paola Minghetti, Francesca Romana Mendicino, Luana Perioli, Maurizio Ricci Manufacturing is the bridge between research and patient: without product, there is no clinical outcome. Shortage has a variety of causes, in this paper we analyse only causes related to manufacturing technology and we use shortage as a paradigm highliting the relevance of Pharmaceutical Technology. Product and process complexity and capacity...
Source: International Journal of Pharmaceutics - November 17, 2016 Category: Drugs & Pharmacology Source Type: research

New nano-matrix oral formulation of nanoprecipitated cyclosporine A prepared with multi-inlet vortex mixer
We present a combined nanoparticle (NP) formation process and spray drying to create a nano-matrix formulation of cyclosporine A (CsA) and mannitol (nCsA/MAN) to increase the bioavailability of CsA. CsA NPs were prepared by flash nano precipitation (FNP) using a multi-inlet vortex mixer, and spray-dried with or without mannitol to prepare nCsA/MAN or nanoprecipitated CsA powder (nCsA), respectively. Pre-forming the NPs by FNP uncouples the sizes of the CsA inclusions from the ultimate micron-sized powders produced by spray drying. Both CsA formulations were physicochemically characterized, and a pharmacokinetic study in ra...
Source: International Journal of Pharmaceutics - November 16, 2016 Category: Drugs & Pharmacology Source Type: research

In-situ single pass intestinal permeability and pharmacokinetic study of developed Lumefantrine loaded solid lipid nanoparticles
Publication date: 10 January 2017 Source:International Journal of Pharmaceutics, Volume 516, Issues 1–2 Author(s): Anuj Garg, Kripal Bhalala, Devendra Singh Tomar, Wahajuddin The present investigation aims to develop lumefantrine loaded binary solid lipid nanoparticles (LF-SLNs) to improve its poor and variable oral bioavailability. The oral bioavailability of LF is poor and variable due to its limited aqueous solubility and P-gp mediated efflux occurring in small intestine. LF-SLNs were prepared using binary lipid mixture of stearic acid and caprylic acid stabilized with TPGS (D-alpha tocopheryl polyethylene glycol...
Source: International Journal of Pharmaceutics - November 16, 2016 Category: Drugs & Pharmacology Source Type: research

Polysaccharide-coated liposomal formulations for dental targeting
Publication date: 10 January 2017 Source:International Journal of Pharmaceutics, Volume 516, Issues 1–2 Author(s): Sara Pistone, Morten Rykke, Gro Smistad, Marianne Hiorth The efficacy of treatments of oral ailments is often challenged by a low residence time of the conventional pharmaceutical formulations in the oral cavity, which could be improved by using bioadhesive formulations. This in vitro study investigated charged liposomes, both uncoated and coated through electrostatic deposition with polysaccharides (chitosan, alginate and pectin), as bioadhesive systems for the oral cavity. First, formulations that pro...
Source: International Journal of Pharmaceutics - November 16, 2016 Category: Drugs & Pharmacology Source Type: research

Microfluidics platform for glass capillaries and its application in droplet and nanoparticle fabrication
Publication date: 10 January 2017 Source:International Journal of Pharmaceutics, Volume 516, Issues 1–2 Author(s): Bárbara Herranz-Blanco, Eloy Ginestar, Hongbo Zhang, Jouni Hirvonen, Hélder A. Santos The accessibility to microfluidics of a broader scientific community is often limited by the costly and complex manufacture of the chips. In this respect, we present a simple and reusable platform for the flexible and easy assembly of glass capillaries to create a microfluidics chip within minutes, with excellent chemical compatibility and durability, and without the need of using specialized infrastructu...
Source: International Journal of Pharmaceutics - November 16, 2016 Category: Drugs & Pharmacology Source Type: research

Impact of additives on the formation of protein aggregates and viscosity in concentrated protein solutions
Publication date: 10 January 2017 Source:International Journal of Pharmaceutics, Volume 516, Issues 1–2 Author(s): Katharina Christin Bauer, Susanna Suhm, Anna Katharina Wöll, Jürgen Hubbuch In concentrated protein solutions attractive protein interactions may not only cause the formation of undesired aggregates but also of gel-like networks with elevated viscosity. To guarantee stable biopharmaceutical processes and safe formulations, both phenomenons have to be avoided as these may hinder regular processing steps. This work screens the impact of additives on both phase behavior and viscosity of concentra...
Source: International Journal of Pharmaceutics - November 16, 2016 Category: Drugs & Pharmacology Source Type: research

Microfluidic manufacturing of phospholipid nanoparticles: Stability, encapsulation efficacy, and drug release
In this study, the microfluidic method for liposomes preparation is presented. DMPC and DSPC liposomes containing two different lipid/cholesterol ratios (1:1 and 2:1) are prepared. Results from this preparation process were compared with the film hydration method in order to understand benefits and drawbacks of microfluidics. Liposomes characterisation was evaluated through stability studies, encapsulation efficacy and drug release profiles of hydrophilic and lipophilic compounds. Stability tests were performed during 3 weeks and the liposomes properties of the most stable formulations were determined using Infrared Micros...
Source: International Journal of Pharmaceutics - November 15, 2016 Category: Drugs & Pharmacology Source Type: research

Improved formulation of cationic solid lipid nanoparticles displays cellular uptake and biological activity of nucleic acids
Publication date: 10 January 2017 Source:International Journal of Pharmaceutics, Volume 516, Issues 1–2 Author(s): Anna Fàbregas, Silvia Prieto, Marc Suñé-Pou, Sofía Boyero-Corral, Josep Ramón Ticó, Encarna García-Montoya, Pilar Pérez-Lozano, Montserrat Miñarro, Josep Mª Suñé-Negre, Cristina Hernández-Munain, Carlos Suñé Non-viral delivery using cationic solid lipid nanoparticles (SLNs) represents a useful strategy to introduce large DNA and RNA molecules to target cells. A careful selection of components and their...
Source: International Journal of Pharmaceutics - November 15, 2016 Category: Drugs & Pharmacology Source Type: research

Formulation and comparative in vitro evaluation of various dexamethasone-loaded pH-sensitive polymeric nanoparticles intended for dermal applications
In conclusion, various pH-sensitive nanoparticles that could release differently on the skin surface and dissolve and release in the hair follicles were obtained. Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - November 15, 2016 Category: Drugs & Pharmacology Source Type: research

Folic acid-decorated and PEGylated PLGA nanoparticles for improving the antitumour activity of 5-fluorouracil
Publication date: 10 January 2017 Source:International Journal of Pharmaceutics, Volume 516, Issues 1–2 Author(s): Mazen M. El-Hammadi, Ángel V. Delgado, Consolación Melguizo, José C. Prados, José L. Arias 5-Fluorouracil (5-FU) is a broad spectrum cytotoxic agent being used in chemotherapy of malignancies. However, 5-FU shows a number of limitations like short half-life, non-selective biodistribution, and the development of drug resistances by tumour cells. It was investigated the potential use of folic acid-decorated and PEGylated poly(D,L-lactide-co-glycolide) nanoparticles (FOL-PEG-PLG...
Source: International Journal of Pharmaceutics - November 15, 2016 Category: Drugs & Pharmacology Source Type: research

The effects of hydration media on the characteristics of non-ionic surfactant vesicles (NISV) prepared by microfluidics
Publication date: 10 January 2017 Source:International Journal of Pharmaceutics, Volume 516, Issues 1–2 Author(s): Mohammad A. Obeid, Ibrahim Khadra, Alexander B. Mullen, Rothwelle J. Tate, Valerie A. Ferro Non-ionic surfactant vesicles (NISV) are colloidal particles that provide a useful delivery system for drugs and vaccines. One of the methods that is used for NISV preparation is microfluidics in which the lipid components dissolved in organic phase are mixed with an aqueous medium to prepare the particles through self-assembly of the lipids. In this work, we examined the effect of using different types of aqueou...
Source: International Journal of Pharmaceutics - November 15, 2016 Category: Drugs & Pharmacology Source Type: research

Ionic liquids as potential enhancers for transdermal drug delivery
Publication date: 10 January 2017 Source:International Journal of Pharmaceutics, Volume 516, Issues 1–2 Author(s): Daniela Monti, Emanuele Egiziano, Susi Burgalassi, Patrizia Chetoni, Cinzia Chiappe, Angelo Sanzone, Silvia Tampucci The aim of this study was to verify the effect of several cyclic onium based ionic liquids (ILs), including mono- and dicationic derivatives of 1,4-diazabicyclo[2.2.2]octane (DABCO), a dialkyl morpholinium salt and a Brønsted acidic IL, as enhancers of the in vitro transdermal permeation and skin retention of diltiazem through and into hairless rat skin. The drug was used as both t...
Source: International Journal of Pharmaceutics - November 15, 2016 Category: Drugs & Pharmacology Source Type: research

Development of near zero-order release PLGA-based microspheres of a novel antipsychotic
Publication date: 10 January 2017 Source:International Journal of Pharmaceutics, Volume 516, Issues 1–2 Author(s): Jinlong Zhao, Lexi Wang, Chunyu Fan, Kongtong Yu, Ximing Liu, Xiaolei Zhao, Dan Wang, Wenhua Liu, Zhengxing Su, Fengying Sun, Youxin Li The novel antipsychotic isoperidone, a prodrug of paliperidone, was designed to improve liposolubility for the development of poly(D,L-lactide-co-glycolide) (PLGA)-based microspheres to achieve near zero-order release behaviour in vivo. Microspheres with a smooth surface were obtained using the oil-in-water emulsion solvent evaporation method and yielded a high encapsul...
Source: International Journal of Pharmaceutics - November 15, 2016 Category: Drugs & Pharmacology Source Type: research

The effect of material attributes and process parameters on the powder bed uniformity during a low-dose dosator capsule filling process
The objective of this work was to assess the effect of process parameters of a dosator nozzle machine on the powder bed uniformity of inhalation powders with various characteristics during a low-dose dosator capsule filling process. Three grades of lactose excipients were extensively characterized and filled into size 3 capsules using different dosing chamber lengths (2.5, 5mm), nozzle diameters (1.9, 3.4mm), powder bed heights (5, 10mm) and filling speeds (500, 3000capsules/h). The fill weight and the weight variability of Lactohale 100 (large particles, good flowability, low cohesion) remained almost the same, regardless...
Source: International Journal of Pharmaceutics - November 15, 2016 Category: Drugs & Pharmacology Source Type: research

Polymeric particle-mediated molecular therapies to treat spinal cord injury
Publication date: 10 January 2017 Source:International Journal of Pharmaceutics, Volume 516, Issues 1–2 Author(s): Farideh Ordikhani, Saahil Sheth, Silviya Petrova Zustiak Spinal cord injury (SCI) is a physically and psychologically debilitating condition that mainly affects young, healthy males who are at the peak of their personal and professional development. SCI damages axons and disrupts myelination, which interrupts sensory and motor neuronal function. Current treatments are mostly palliative, aimed at reducing further damage and pain, but do not provide a cure. Polymeric particles have shown tremendous promis...
Source: International Journal of Pharmaceutics - November 15, 2016 Category: Drugs & Pharmacology Source Type: research

Poly vinyl acetate and ammonio methacrylate copolymer as unconventional polymer blends increase the mechanical robustness of HPMC matrix tablets
Conclusion Poly vinyl acetate and ammonio methacrylate copolymer could be a proper polymer blend for coating HPMC matrix tablets to increase mechanical robustness, which characterized by its flexibility and permeability. Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - November 14, 2016 Category: Drugs & Pharmacology Source Type: research

Osmolality of antisense oligonucleotide parenteral formulations: Implications on counterion dissociation and recommended osmometry techniques
Publication date: 30 December 2016 Source:International Journal of Pharmaceutics, Volume 515, Issues 1–2 Author(s): Marc Lim, Andrew Dibble The intrinsic osmolality of aqueous solutions of sodium salt antisense oligonucleotides (ASOs) has been studied to inform formulation practices, understand the molecular basis underlying the difference between theoretical and empirical results, and determine suitable measurement methods. It was found that regardless of nucleotide sequence, ASO concentration of ∼140mg/mL has isotonic osmolality of ∼290mOsm/kg water (SI unit: mmol osmotically-active particles/kg water), su...
Source: International Journal of Pharmaceutics - November 12, 2016 Category: Drugs & Pharmacology Source Type: research

Evaluation of Pentravan ®, Pentravan® Plus, Phytobase®, Lipovan® and Pluronic Lecithin Organogel for the transdermal administration of antiemetic drugs to treat chemotherapy-induced nausea and vomiting at the hospital
The objective of this study was to evaluate five commercial ready-to-use transdermal vehicles (Phytobase®, Lipovan®, Pentravan®, Pentravan® Plus and Pluronic Lecithin Organogel (PLO)), for the compounding of three antiemetic drugs (ondansetron, dexamethasone and aprepitant) and their administration in combination to treat chemotherapy-induced nausea and vomiting (CINV) at the hospital. Drugs were individually formulated in these vehicles and in mixture in Pentravan® Plus using different penetration enhancers. Quality control of the forms has demonstrated that formulation process was mastered and conveni...
Source: International Journal of Pharmaceutics - November 12, 2016 Category: Drugs & Pharmacology Source Type: research

Style and precision in scientific papers
Publication date: 10 January 2017 Source:International Journal of Pharmaceutics, Volume 516, Issues 1–2 Author(s): Alexander T. Florence (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - November 12, 2016 Category: Drugs & Pharmacology Source Type: research

Efficient approach to enhance drug solubility by particle engineering of bovine serum albumin
Publication date: 30 December 2016 Source:International Journal of Pharmaceutics, Volume 515, Issues 1–2 Author(s): Mouhamad Khoder, Hamdy Abdelkader, Amr ElShaer, Ayman Karam, Mohammad Najlah, Raid G. Alany The aim of this study was to investigate the use of bovine serum albumin (BSA) as a solubility enhancer for indometacin (IND) as a model drug. IND-BSA solid dispersions were prepared by both spray drying and freeze drying techniques using IND:BSA solution (20:1 Molar Ratio (MR)) and IND:BSA suspension (100:1 MR). The solid state of IND in solid dispersions was characterised by SEM, DSC and XRD. The aqueous solub...
Source: International Journal of Pharmaceutics - November 10, 2016 Category: Drugs & Pharmacology Source Type: research

Where does hydrolysis of nandrolone decanoate occur in the human body after release from an oil depot?
Publication date: 30 December 2016 Source:International Journal of Pharmaceutics, Volume 515, Issues 1–2 Author(s): R.W. Kalicharan, M.R. Bout, C. Oussoren, H. Vromans Long-term therapy of nandrolone (N) is recommended to increase mineral density and muscle strength. Using a parenteral sustained release drug formulation with nandrolone decanoate (ND), therapeutic N levels can be achieved and maintained. Until now, it is unknown if hydrolysis of ND into N occurs in tissue at the injection site or after systemic absorption. Therefore, hydrolysis studies were conducted to investigate the location and rate of ND hydroly...
Source: International Journal of Pharmaceutics - November 10, 2016 Category: Drugs & Pharmacology Source Type: research

Impact of sodium chloride on the expansion of a liquid-liquid miscibility gap in an API/water system. Case study of Brivaracetam
Publication date: 30 December 2016 Source:International Journal of Pharmaceutics, Volume 515, Issues 1–2 Author(s): Nicolas Couvrat, Julien Mahieux, Baptiste Fours, Yohann Cartigny, Eric Schenkel, Luc Aerts, Luc Quéré, Gérard Coquerel Brivaracetam, or (2S)-2-[(4R)-2-oxo-4-propyl-pyrrolidin-1-yl] butanamide, is an active pharmaceutical ingredient designed for the treatment of epilepsy. During the development of the IV administration mode, a liquid-liquid miscibility gap has been observed with pure water, isotonic and hypertonic solutions (vehicle at 0.9% w/w and 5%w/w NaCl respectively). The stud...
Source: International Journal of Pharmaceutics - November 10, 2016 Category: Drugs & Pharmacology Source Type: research

Encapsulation of NSAIDs for inflammation management: Overview, progress, challenges and prospects
Publication date: 30 December 2016 Source:International Journal of Pharmaceutics, Volume 515, Issues 1–2 Author(s): Waisudin Badri, Karim Miladi, Qand Agha Nazari, Hélène Greige-Gerges, Hatem Fessi, Abdelhamid Elaissari Non-steroidal anti-inflammatory drugs (NSAIDs) are among the most widely prescribed drugs. Debilitating diseases such as rheumatoid arthritis and osteoarthritis are commonly managed by NSAIDs. However, NSAIDs pharmacological mechanism is often associated with the presence of gastrointestinal side effects. NSAIDs encapsulation is performed in order to overcome some of the drawbacks linke...
Source: International Journal of Pharmaceutics - November 10, 2016 Category: Drugs & Pharmacology Source Type: research

Oral sustained-release suspension based on a lauryl sulfate salt/complex
The objective of this study was to evaluate the feasibility of lauryl sulfate (LS) salt/complex as a novel carrier in oral sustained-release suspensions. Mirabegron, which has a pH-dependent solubility, was selected as the model drug. Sodium lauryl sulfate (SLS) was bound to mirabegron in a stoichiometric manner to form an LS salt/complex. LS salt/complex formulation significantly reduced the solubility of mirabegron and helped mirabegron achieve sustained-release over a wide range of pH conditions. Microparticles containing the LS salt/complex were prepared by spray drying with the aqueous dispersion of ethylcellulose (Aq...
Source: International Journal of Pharmaceutics - November 8, 2016 Category: Drugs & Pharmacology Source Type: research

Complexation of curcumin with 2-aminoethyl diphenyl borate and implications for spatiotemporal fluorescence monitoring
In this study, we successfully determined spatiotemporal distribution of curcumin in mice via simple and fast fluorescence detection of native curcumin and stabilized curcumin. We used 2-aminoethyl diphenyl borate (DPBA) as a stabilizer of curcumin, which binds to curcumin and enhances its aqueous stability. After intravenous injection, curcumin and DPBA–curcumin complexes showed similar fluorescence intensities in the brain, pancreas, lungs, and kidneys at 15min. However, stabilized DPBA–curcumin complexes exhibited much stronger fluorescent signals at metabolically active sites such as liver tissues than nati...
Source: International Journal of Pharmaceutics - November 8, 2016 Category: Drugs & Pharmacology Source Type: research

Rapid and cost-effective xenograft hepatocellular carcinoma model in Zebrafish for drug testing
In conclusion, the possibility to test anti HCC/neo-angiogenesis drugs makes our JHH6 model useful to select therapeutic molecules for a highly vascularized tumor such as HCC. Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - November 3, 2016 Category: Drugs & Pharmacology Source Type: research

Preformulation of cysteamine gels for treatment of the ophthalmic complications in cystinosis
In conclusion these results offer the possibility to formulate cysteamine in an ocular applicable gel formulation. Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - November 2, 2016 Category: Drugs & Pharmacology Source Type: research

Porous microscaffolds for 3D culture of dental pulp mesenchymal stem cells
Publication date: 30 December 2016 Source:International Journal of Pharmaceutics, Volume 515, Issues 1–2 Author(s): Ronak S. Bhuptani, Vandana B. Patravale The collective power of stem cells due to their evident advantages is incessantly investigated in regenerative medicine to be the next generation exceptional remedy for tissue regeneration and treatment of diseases. Stem cells are highly sensitive and a 3D culture environment is a requisite for its successful transplantation and integration with tissues. Porous microscaffolds can create a 3D microenvironment for growing stems cells, controlling their fate both in...
Source: International Journal of Pharmaceutics - November 2, 2016 Category: Drugs & Pharmacology Source Type: research

Gellan gum fluid gels for topical administration of diclofenac
This study highlights the potential use of fluid gels that can be easily tuned to have physical properties suitable for topical formulations with the added advantage of increasing drug permeation. Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - November 2, 2016 Category: Drugs & Pharmacology Source Type: research

Albumin hybrid nanoparticles loaded with tyrosine kinase A inhibitor GNF-5837 for targeted inhibition of breast cancer cell growth and invasion
Publication date: 30 December 2016 Source:International Journal of Pharmaceutics, Volume 515, Issues 1–2 Author(s): Vahid Heravi Shargh, Hubert Hondermarck, Mingtao Liang Novel albumin hybrid nanoparticles (Alb-HNPs) loaded with tyrosine kinase A (TrkA) inhibitor GNF-5837 were prepared and evaluated for antineoplastic efficacy in a panel of breast cancer cell lines. The nanomedicines (GNF-Alb-HNPs, hydrodynamic diameter ∼150nm) were formed through a unique polyelectrolyte complexation process where albumin and GNF-5837 were encapsulated by a stabilizing layer of oppositely charged chitosan and dextran sulfate po...
Source: International Journal of Pharmaceutics - November 2, 2016 Category: Drugs & Pharmacology Source Type: research

Miktoarm star copolymers from D-( −)-salicin core aggregated into dandelion-like structures as anticancer drug delivery systems: synthesis, self-assembly and drug release
Publication date: 30 December 2016 Source:International Journal of Pharmaceutics, Volume 515, Issues 1–2 Author(s): Anna Mielańczyk, Justyna Odrobińska, Sebastian Grządka, Łukasz Mielańczyk, Dorota Neugebauer The β-glucoside-based heterofunctional initiator was used in the synthesis of well-defined eight-armed miktopolymers by sequential ring opening polymerization (ROP) of ε-caprolactone (CL) and atom transfer radical (co)polymerization (ATRP) of methyl methacrylate (MMA) and/or tert-butyl methacrylate (tBMA). Consequently, methacrylic acid (MAA) repeating units were introduced via selective cleav...
Source: International Journal of Pharmaceutics - November 2, 2016 Category: Drugs & Pharmacology Source Type: research

Nanoemulsion enhances α-tocopherol succinate bioavailability in rats
In conclusion, our laboratory-made NE was a safe drug delivery system for clinical trials and could be a promising formulation for α-TOS by I.V administration. Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - November 2, 2016 Category: Drugs & Pharmacology Source Type: research

The use of surfactants to enhance the solubility and stability of the water-insoluble anticancer drug SN38 into liquid crystalline phase nanoparticles
Publication date: 30 December 2016 Source:International Journal of Pharmaceutics, Volume 515, Issues 1–2 Author(s): Abdul-Hackam Ranneh, Yasunori Iwao, Shuji Noguchi, Toshihiko Oka, Shigeru Itai Cubosomes were used to increase the aqueous solubility of the water insoluble anticancer drug SN38. The results showed that the use of a common cubosome formulation consisting of phytantriol (PHYT) as the matrix amphiphile (PHYT-cubosome) led to a 6-fold increase in the solubility of SN38. However, mean hydrodynamic diameter (D H) and polydispersity index (PDI) of these PHYT-cubosome particles were 345±49nm and 0.37&p...
Source: International Journal of Pharmaceutics - October 29, 2016 Category: Drugs & Pharmacology Source Type: research

Controlled drug release from hydrogels for contact lenses: Drug partitioning and diffusion
Publication date: 30 December 2016 Source:International Journal of Pharmaceutics, Volume 515, Issues 1–2 Author(s): A.F.R. Pimenta, J. Ascenso, J.C.S. Fernandes, R. Colaço, A.P. Serro, B. Saramago Optimization of drug delivery from drug loaded contact lenses assumes understanding the drug transport mechanisms through hydrogels which relies on the knowledge of drug partition and diffusion coefficients. We chose, as model systems, two materials used in contact lens, a poly-hydroxyethylmethacrylate (pHEMA) based hydrogel and a silicone based hydrogel, and three drugs with different sizes and charges: chlorhexidi...
Source: International Journal of Pharmaceutics - October 27, 2016 Category: Drugs & Pharmacology Source Type: research

Polysialic acid-modifying liposomes for efficient delivery of epirubicin, in-vitro characterization and in-vivo evaluation
In this study, PSA was conjugated with octadecyl dimethyl betaine (BS18) to yield a PSA-BS18 conjugate. The PSA-BS18 modified liposomal epirubicin (EPI-SL), had a particle size of 133.63±0.92nm, a zeta potential of −26.23±1.50mV and an encapsulation efficiency (%EE) of 96.23±1.16%. In vitro release studies showed that PSA-BS18 could delay EPI release from the modified liposomes. The MTT assay suggested that EPI-SL led to stronger cytotoxic activity than that exhibited by common and PEGylated liposomes. The pharmacokinetic study showed that EPI-SL prolonged the residence time of the EPI in the blo...
Source: International Journal of Pharmaceutics - October 27, 2016 Category: Drugs & Pharmacology Source Type: research

Development of a novel oral delivery system of edaravone for enhancing bioavailability
Publication date: 30 December 2016 Source:International Journal of Pharmaceutics, Volume 515, Issues 1–2 Author(s): Ankit Parikh, Krishna Kathawala, Chun Chuan Tan, Sanjay Garg, Xin-Fu Zhou Edaravone (EDR), a strong free radical scavenger, is known for its promising therapeutic potential in oxidative stress (OS) associated diseases, however poor oral bioavailability is the major obstacle in its potential use. Oral liquid dosage form is the most preferred delivery method in paediatric, geriatric and specialised therapies. The present research discusses the development of a Novel Oral Delivery System (NODS) of EDR to ...
Source: International Journal of Pharmaceutics - October 27, 2016 Category: Drugs & Pharmacology Source Type: research

Enhanced oral delivery of alendronate by sucrose fatty acids esters in rats and their absorption-enhancing mechanisms
Publication date: 30 December 2016 Source:International Journal of Pharmaceutics, Volume 515, Issues 1–2 Author(s): Tammam Alama, Hiroko Katayama, Sachiko Hirai, Shizuka Ono, Ayumi Kajiyama, Kosuke Kusamori, Hidemasa Katsumi, Toshiyasu Sakane, Akira Yamamoto Oral delivery is the most fascinating route for interminable drug remedy. However, the intestinal absorption of alendronate (ALN), a bisphosphonate drug after oral administration is very poor. Absorption enhancers, which help to achieve the efficiency-safety balance, are considered one of the most promising agents for the improvement the intestinal absorption of...
Source: International Journal of Pharmaceutics - October 27, 2016 Category: Drugs & Pharmacology Source Type: research

Drug-eluting coating of ginsenoside Rg1 and Re incorporated poly(lactic-co-glycolic acid) on stainless steel 316L: Physicochemical and drug release analyses
Publication date: 30 December 2016 Source:International Journal of Pharmaceutics, Volume 515, Issues 1–2 Author(s): Zulaika Miswan, Siti Khadijah Lukman, Fadzilah Adibah Abd Majid, Mun Fai Loke, Syafiqah Saidin, Hendra Hermawan Active ingredients of ginsenoside, Rg1 and Re, are able to inhibit the proliferation of vascular smooth muscle cells and promote the growth of vascular endothelial cells. These capabilities are of interest for developing a novel drug-eluting stent to potentially solve the current problem of late-stent thrombosis and poor endotheliazation. Therefore, this study was aimed to incorporate ginseno...
Source: International Journal of Pharmaceutics - October 27, 2016 Category: Drugs & Pharmacology Source Type: research

Impact of sodium lauryl sulfate in oral liquids on e-tongue measurements
Publication date: 30 December 2016 Source:International Journal of Pharmaceutics, Volume 515, Issues 1–2 Author(s): Laura Isabell Immohr, Roy Turner, Miriam Pein-Hackelbusch During development of oral liquid medicines taste assessment is often required to evaluate taste and taste masking. Electronic tongue analysis can provide taste assessment of medicinal products but should only be conducted with medicines that interact with the instrument without damaging the sensor membranes or interfering with their electrical output so that robust data is generated. To explore the impact of a substance deemed unsuitable for el...
Source: International Journal of Pharmaceutics - October 27, 2016 Category: Drugs & Pharmacology Source Type: research

CXCR4-targeted modular peptide carriers for efficient anti-VEGF siRNA delivery
Publication date: 30 December 2016 Source:International Journal of Pharmaceutics, Volume 515, Issues 1–2 Author(s): Anna Egorova, Anastasia Shubina, Dmitriy Sokolov, Sergey Selkov, Vladislav Baranov, Anton Kiselev The application of small interfering RNA (siRNA) for specific gene inhibition is a promising strategy in gene therapy treatments. The efficient cellular delivery of therapeutic siRNA is a critical step in RNA interference (RNAi) application. Highly efficient siRNA carriers should be developed for specific cellular uptake, stable RNA-complexes formation and intracellular RNA release. To study these features...
Source: International Journal of Pharmaceutics - October 26, 2016 Category: Drugs & Pharmacology Source Type: research

Delivery system for berberine chloride based on the nanocarrier ZnAl-layered double hydroxide: Physicochemical characterization, release behavior and evaluation of anti-bacterial potential
Publication date: 30 December 2016 Source:International Journal of Pharmaceutics, Volume 515, Issues 1–2 Author(s): Mohamed Amine Djebbi, Alae Elabed, Zaineb Bouaziz, Moulay Sadiki, Soumya Elabed, Philippe Namour, Nicole Jaffrezic-Renault, Abdesslem Ben Haj Amara Layered double hydroxide (LDH) has attracted major interest as one of the most versatile drug delivery systems especially for adsorption capacity and/or controlled delivery property of bioactive agents owing to their combining features of biohybrid. ZnAl synthesized layered double hydroxide can offer a platform to immobilize various types of bioactive compo...
Source: International Journal of Pharmaceutics - October 25, 2016 Category: Drugs & Pharmacology Source Type: research

The effect of structurally related impurities on crystallinity reduction of sulfamethazine by grinding
In this study, the effect of structurally related impurities on crystallinity reduction of sulfamethazine by grinding was evaluated. The crystallinity of sulfamethazine was not decreased when it was ground alone. However, when structurally related impurities with sulfonamide derivatives were blended, the crystallinity of sulfamethazine was decreased by grinding. Other materials without a sulfonamide moiety showed no such effect. The Raman spectra of sulfamethazine demonstrated that there was a difference between its crystalline and amorphous states within its sulfonamide structure. It was suggested that the sulfonamide str...
Source: International Journal of Pharmaceutics - October 24, 2016 Category: Drugs & Pharmacology Source Type: research

In vivo skin penetration of macromolecules in irritant contact dermatitis
In conclusion, the changes in skin permeability accompanied with skin inflammation did not affect its permeability to peptide drugs. Our findings also underline that experiments with the tape stripped skin model as a surrogate for inflamed skin can risk misleading conclusions due to significant difference of skin permeability between the tape stripped skin and inflamed skin. Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - October 21, 2016 Category: Drugs & Pharmacology Source Type: research

Juglone loaded poloxamer 188/phospholipid mixed micelles evaluated in vitro and in vivo in breast cancer
Conclusion J-MM exhibited low toxicity, improved cellular uptake, passive targeting and anti-cancer effects in breast cancer model. Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - October 21, 2016 Category: Drugs & Pharmacology Source Type: research

Multispectral UV imaging for surface analysis of MUPS tablets with special focus on the pellet distribution
In conclusion, this study revealed that UV imaging in combination with multivariate image analysis is a promising approach for the automatic quality control of MUPS tablets during the manufacturing process. Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - October 21, 2016 Category: Drugs & Pharmacology Source Type: research